Aromatic, heterocyclic and cycloalkyl carboxylates of the 4-piperidinol system and related tertiary aminoalcohols have been synthesized for pharmacological and biochemical study. Two CNS classes have been found: (1) non-addicting analgesics (mice, Rhesus monkeys); (2) antiepileptics (mice). A tritiated piperidinol ester has been prepared for non-opiate receptor study. Certain compounds have been selected for the study of their effect on the Na ion/K ion channels of electrogenic membranes. Quantitative and qualitative structure-activity relationships have been made.